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  2. Protein Tyrosine Kinase/RTK
  3. VEGFR PDGFR c-Kit
  4. Telatinib mesylate

Telatinib mesylate  (Synonyms: Bay 57-9352 mesylate)

目錄號: HY-10527C 純度: 99.74%
COA 產(chǎn)品使用指南

Telatinib mesylate (Bay 57-9352 mesylate) 是一種有效的的口服活性的 VEGFR2，VEGFR3，PDGFα 和 c-Kit 抑制劑，IC50 分別為 6 nM，4 nM，15 nM 和 1 nM。

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Telatinib mesylate Chemical Structure

Telatinib mesylate Chemical Structure

CAS No. : 332013-26-0

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Customer Review

Other Forms of Telatinib mesylate:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively[1].

IC50 & Target[1]

VEGFR2

6 nM (IC50)

VEGFR3

4 nM (IC50)

PDGFRα

15 nM (IC50)

c-Kit

1 nM (IC50)

體外研究
(In Vitro)

Telatinib enhances the anticancer activity of ABCG2 substrate anticancer drugs by inhibiting ATP-binding cassette G2 (ABCG2) efflux transporter activity. Co-incubation of ABCG2-overexpressing drug resistant cell lines with Telatinib and ABCG2 substrate anticancer drugs significantly reduces cellular viability, whereas Telatinib alone does not significantly affect drug sensitive and drug resistant cell lines. Telatinib at 1 μM does not significantly alter the expression of ABCG2 in ABCG2-overexpressing cell lines. Telatinib at 1 μM significantly enhances the intracellular accumulation of [3H]-mitoxantrone (MX) in ABCG2-overexpressing cell lines[2].
Telatinib at 1 μM significantly reduces the rate of [3H]-MX efflux from ABCG2-overexpressing cells. Furthermore, Telatinib significantly inhibits ABCG2-mediated transport of [3H]-E?17βG in ABCG2 overexpressing membrane vesicles[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Telatinib (15 mg/kg; oral dministration; every 2nd and 3rd day; total 12 times; male athymic NCR (nu/nu) nude mice) with Doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic NCR (nu/nu) nude mice (13-15 g, age 4-5 weeks) injected with H460 and H460/MX20 cells[2]
Dosage: 15 mg/kg
Administration: Oral dministration; every 2nd and 3rd day; total 12 times
Result: With Doxorubicin (1.8 mg/kg) significantly decreased the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model.
Clinical Trial
分子量

505.93

Formula

C21H20ClN5O6S
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

甲磺酸替拉替尼；甲磺酸特拉替尼
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 250 mg/mL (494.14 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9766 mL 9.8828 mL 19.7656 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9766 mL 9.8828 mL 19.7656 mL 49.4140 mL
5 mM 0.3953 mL 1.9766 mL 3.9531 mL 9.8828 mL
10 mM 0.1977 mL 0.9883 mL 1.9766 mL 4.9414 mL
15 mM 0.1318 mL 0.6589 mL 1.3177 mL 3.2943 mL
20 mM 0.0988 mL 0.4941 mL 0.9883 mL 2.4707 mL
25 mM 0.0791 mL 0.3953 mL 0.7906 mL 1.9766 mL
30 mM 0.0659 mL 0.3294 mL 0.6589 mL 1.6471 mL
40 mM 0.0494 mL 0.2471 mL 0.4941 mL 1.2353 mL
50 mM 0.0395 mL 0.1977 mL 0.3953 mL 0.9883 mL
60 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8236 mL
80 mM 0.0247 mL 0.1235 mL 0.2471 mL 0.6177 mL
100 mM 0.0198 mL 0.0988 mL 0.1977 mL 0.4941 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Telatinib mesylate
目錄號：
HY-10527C
需求量：